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PHAMACOLOGY - Cardiology > CV Stimulants > Flashcards

CV Stimulants Flashcards

1
Q

Epinephrine (E)
• Receptors
• Effects
• Uses

A

Epinephrine

Receptors:
• alpha1=alpha2; ß1=ß2

Effects:
• Binds BOTH beta and alpha to cause HTN and rapid HR (respectively)

Uses:
• Anaphylaxis
• Cadiac Arrest
• Hypotension

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2
Q

Norepinephrine (NE)
• Receptors
• Effects
• Uses

A

Norepinephrine

Receptors:
• alpha1 > alpha2 > ß1

Effects:
• binds alpha mainly so you only get HTN

Uses:
• Hypotension (DECREASES RENAL PERFUSION)

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3
Q

Dopamine (DA)
• Receptors
• Effects
• Uses

A

Dopamine

Receptors:
D1=D2 > ß > alpha

Effects:
• binds ß and alpha at HIGH CONC. causing Rapid HR and HTN (respectively)

Uses:
• Unstable Bradycardia, Heart Failure, Shock
• Chronotropic Effects predominate at high Dose

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4
Q

Dobutamine
• Receptors
• Effects
• Uses

A

Dobutamine

Receptors:
• ß1 > ß2, alpha

Effect:
• Binds ß and alpha to cause Rapid HR and HTN (respectively)

Uses:
• Heart Failure (inotropic > chronotropic)
• Stress Tests

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5
Q

Isoproterenol [Isuprel]
• Receptors
• Effects
• Uses

A

Isoproterenol

Receptors:
• ß1 = ß2

Effect:
• Binds ß to cause rapid HR

Uses:
• Electrophysiologic Evaluation of Tachyarrythmia
• Can worsen ischemia

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6
Q

Phenylephrine
• Receptors
• Effects
• Uses

A

Phenylephrine

Receptors:
• alpha1 > alpha 2

Effect:
• Binds alpha to cause HTN

Uses:
• Hypotension

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7
Q

Ephedrine [Pretz-D]
• Receptors
• Effects
• Uses

A

Ephedrine

Receptors:
• alpha 1 > alpha2 > ß1

Effect:
• INDIRECT activation of alpha and beta cause HTN and increased HR (respectively)

Uses: 
• Hypotension of anesthesia
• Narcolepsy
• Nasal Congestion
• Asthma
• Bronchospasm
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8
Q

What is the effect of stimulating Beta-1 receptors?

• where are these found?

A

Location: Primarily found in Cardiovascular System

Effect: Accelerate Heart Rate and Increase the force of contraction

Uses:

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9
Q

What is the effect of stimulating Beta-2 receptors?

• where are these found?

A

Location: Beta-2 found in Skeletal muscle (also they are found in CV system with Beta-1 receptors)

Effect: stimulation leads to muscle relaxation and increased perfusion

Uses:

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10
Q

What is the difference in Direct-acting and Indirect acting Sympathomimetic Drugs?

A

Direct:
• acts on the POST-Synaptic membrane to stimulate the receptor Directly

Indirect:
• Increase Availability of NE (norepinephrine) and E (epinephrine) by acting on the PRE-SYNAPIC neuron

Mixed:
• Direct activation on Post-synaptic and stimulation of Neurotransmitter release from PRE-synaptic neuron

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11
Q

In what ways can drugs indirectly act on neurons?

A
  • Releasing or Displacing NE
  • Blocking NE transport into sympathetic neurons
  • Blocking metabolizing enzymes (Monamine oxidase, MAO) or catechol-O-methyltransferase (COMT)
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12
Q

What effect does reserpine on:
• Direct-acting drugs
• Indirectly-acting drugs
• Mixed-acting drugs

A

Direct-acting:
• NO response reduction
• May INCREASE (why?)

Indirectly-acting:
• ABOLISHED responses because there is no NE to stimulate the release of

Mixed:
• Effects will be blunted by reserpine

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13
Q

What does reserpine do?

A

• Reserpine depletes NE (norepinephrine) from sympathetic neurons

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14
Q

Dopamine is dose dependent, what are its effects at the following concetrations:
• Low
• Intermediate
• High

A

Low:
• D1/D2 receptors predominate

Intermediate:
• Beta receptor actions are seen (tachycardia)

High:
• Alpha receptor actions are seen HTN

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15
Q

What are the effects of epinephrine?

• are they dose dependent?

A

***Yes they are dose dependent

Low Dose:
• ß - receptors are predominatly activated
• Increased HR and Decreased Peripheral Resistance (via ß2) WIDEN the Pulse pressure (aka the window between systolic and diastolic)

High Dose:
• alpha - receptors are stimulated

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16
Q

Explain what happens to the following and why, when NE is injected into someone:
• Peripheral Resistance
• Heart Rate
• BP

A

Peripheral Resistance:
• Increased - NE acts mostly on alpha-1 receptors to cause vasocontriction

Heart Rate:
• Decreased - reduced by BARORECEPTOR response to increased resistance

Blood Pressure:
• Both Systolic and Diastolic are raised

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17
Q

Explain what happens to the following and why, when E is injected into someone:
• Peripheral Resistance
• Heart Rate
• BP

A

Peripheral Resistance:
• Decreased - E acts on Beta-2 receptors mostly at low dose cause vasodilation in skeletal muscle

Heart Rate:
• Increased - E acts on Beta-1 receptors stimulating an increased contraction

Blood Pressure:
• Widened HIGHer SYSTOLIC and LOWER Diastolic

18
Q

Explain what happens to the following and why, when Isoproterenol is injected into someone:
• Peripheral Resistance
• Heart Rate
• BP

A

Peripheral Resistance:
• Decreased - E acts on Beta-2 receptors mostly at low dose cause vasodilation in skeletal muscle

Heart Rate:
• Increased - E acts on Beta-1 receptors stimulating an increased contraction

Blood Pressure:
• Widened HIGHer SYSTOLIC and LOWER Diastolic

19
Q

T or F: Isoproterenol and epinephrine have essentially the same effect on BP.

A

False, while the effects are similar isoproterenol is much more potent and widens the Systolic/Diastolic window even more because it has NO ALPHA ACTIVITY

20
Q

Epinephrine
• Routes of Administration
• Adverse Effects
• Uses

A

Routes of Administration:
• Inhaled, IV, or IM

Adverse Effects:
• Cerebral Hemorrhage
• Ventricular Arrhythmias
• Angina

Treats:
• Hypersensitivity Reactions
• Used at Vasocontrictor w/ Local Anesthetics
• Restores cardiac rhythm in cardiac arrest

21
Q

Why is epinephrine not given orally or SC if you want systemic effects?

A

• It vasocontricts really hard so drug cannot travel far

22
Q

Why is administration of epinephrine often contraindicated with beta blockers?
• what adverse effect might be more likely?

A
  • Epinephrine works on both Alpha and Beta receptors

* Vasodilatory effects of beta action helps to prevent insanely high increases in BP caused by alpha action

23
Q

Epinephrine
• Effect on Heart
• Potential Problems

A

Heart:
• Directly stimulates ß-1 receptors

Effect:
INCREASED CO (cardiac output)
• High HR (increased SA node depolarization)
• Increased Amplitude of Action Potential
• Increased Rate of Phase 0 depolarization
• Shortens AV node refractory period

Problems:
• Fibrillation (in company of other drugs)
• Pro-arrhythmogenic

24
Q

How do the effect of NE and E on the SA node differ from that of ACh?
• Why?

A

NE and E:
• Stimulate increased rates of of SA nodal discharge

ACh:
• Decreased the rate of SA nodal discharge by acting through Muscarinic (M2) receptors

25
Q

Epinephrine
• Effect on Vasculature
• Beta-1/2 effects (renal, skeletal mm, coronary)
• Alpha Effects (skin)

A

Overall Sympathetic Effects:
Beta-1 /Beta-2 effects:

  • Beta-1: JGA stimulated => Renin Secretion => renal vascular resistance => Decreased Renal Bloodflow => Na+, K+, Cl- retained
  • Beta-2: Increased Skeletal Muscle Perfusion, Increased Disastole => Increased Coronary Blood Flow
  • Both: Increased cardiac output leads to increased Pulmonary Arterial and Venous pressures

Alpha Effects:
• Decreased Perfusion of the Skin

26
Q

Why does epinephrine shorten systole?

A
  • Shortened Systole increases the duration of diastole

* Heart is perfused during Diastole

27
Q

What is the major difference between NE and E when it comes to the heart?
• why?

A

Norepinephrine:
• Does NOT increase cardiac output (CO)
• NO role in accelerating heart rate - NO BETA-2 action

Epinephrine
• DOES increase CO
• DOES accelerate HR - through BETA-2

28
Q

What is the difference in NE and E with respect to effects on blood pressure?
• why?

A

• Norepinephrine has a stronger effect on blood pressure because there is no Beta-2 action that acts to dilate blood vessels in the periphery

29
Q

Adverse effects of Norepinephrine.

A

Problems:
• Fibrillation (in company of other drugs)
• Pro-arrhythmogenic
• More problems with BP compared to people given E

30
Q

How is norepinephrine Administered?

• Side effects of administration?

A

Administration:
• IV

Side Effects:
• Necrosis at infusion side
• Diminished Organ Blood Flow

31
Q

What are the steps in Epinephrine sythesis starting with tyrosine?

A

Tyrosine => Dopa => Dopamine => Norepinephrine => Epinephrine

32
Q

Dopamine
• Uses/MOA
• Administration
• Fallbacks?

A

Uses/MOA:
• Acts on D1 receptors in the kidney to INCREASE RENAL PERFUSION => urine output will tell you if its working

Administration:
•Given IV

Drawback:
•Can only be given for in patient use because it has a SHORT DURATION OF ACTION and must be given IV

33
Q

Dopamine

•Dose Dependent Effects

A

LOW: D1 action
• RENAL - Increases Perfusion (inc. GFR)

MODERATE: D1 and ß1 action
• Increased Cardiac Output (Contractility&raquo_space; HR)
• Increased NE release from Nerve Terminals b/c of Dopamine stimulation

HIGH: Alpha action mainly
• Increased peripheral Vascular Resistance

34
Q

Dobutamine
• Receptors acted on
• Effect
• Use

A

Receptors:
• ß1-agonist and Alpha-1 agonsit/antagonist (-/+ enantiomers)
• NO ACTIVITY ON DOPAMINE RECEPTORS

Effect:
• Increased Cardiac Output; Increased stroke volume with minimal effect on heart rate

35
Q

How does Dobutamine increase stroke volume without affecting heart rate?

A
  • INCREASED myocardial Contractility
  • DECREASED left ventricular filling pressures
  • INCREASED urinary output
36
Q

Dobutamine
• Administration
• Uses

A

Administration:
• IV infusion
• VERY short T1/2 (2min)

Uses:
• Heart Failure or Acute MI
• Post Cardiac Surgery

37
Q

Isoproterenol:
• Receptors
• Effect

A

Receptors:
• ONLY ACTS on ß1/2 receptors

Effect:
• Increased Cardiac Output
• Decreased Diastolic BP

38
Q

Isoproterenol:
• Uses
• Administration
• Side Effects

A

Uses:
• Stimulates HR in pts. with Bradycardia or Heart Block
• Used in pts. waiting for Pacemakers

Administration:
• Parenteral or by aerosol

Side Effects: 
•Palpitations 
• Tachycardia
• Headache 
• Flushing
39
Q

Phenylephrine
• Receptors
• Effect

A

Receptors
• Alpha agonist (no ß activity)

Effect:
• Increased BP by increasing Systemic Arterial Vasoconstriction
• Reflex Decrease in BP and CO

40
Q

Phenylephrine
• Uses
• Administration
• Adverse effects

A

uses:
• Control Hypotension

Administration:
• SC, IV, IM

Adverse Effects: 
• Angina, Anxiety
• Hallucinations
• HTN
• Insomnia
41
Q

Ephedrine
• MOA
• Effects
• Elimination

A

MOA:
Mixed action
• Enhances NE release from sympathetic neurons
• Direct agonist of Alpha and Beta Receptors

Effects:
•Increased HR and CO
• Increased BP (due to alpha receptor stimulation in vesssels)

Elimination:
• Eliminated Unchanged in the Urine

42
Q

Ephedrine
•Uses
• Adverse Effects

A

uses:
• Hypotension
•Hypotension of Analgesia

Adverse Effects:
• Increased Cardiac Workload => Angina
• Ventricular Dysfunction and Palpitations
• Fatal Arrhythmias

PHAMACOLOGY - Cardiology (11 decks)

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